1. GPCR/G Protein Neuronal Signaling
  2. Melatonin Receptor 5-HT Receptor
  3. TIK-301

TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

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TIK-301 Chemical Structure

TIK-301 Chemical Structure

CAS No. : 118702-11-7

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Description

TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment[1][2][3].

IC50 & Target

melatonin MT1

0.081 nM (Ki)

melatonin MT2

0.042 nM (Ki)

5-HT2C Receptor

 

5-HT2B Receptor

 

In Vivo

In male rats, TIK-301(at doses of 0.8 and 4.0 mg/kg/day) can reduce body weight, and without altering food intake[1][2].
The Tmax and half-life of TIK-301 is 1.1 hour and 1 hour, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

280.75

Formula

C14H17ClN2O2

CAS No.
SMILES

CC(NC[C@@H](C1=CNC2=C1C=C(OC)C(Cl)=C2)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TIK-301
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HY-106136
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